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Your search keyword '"Krainz, Tanja"' showing total 16 results
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16 results on '"Krainz, Tanja"'

1. BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor

Author

Meibom, Daniel, primary, Wasnaire, Pierre, additional, Beyer, Kristin, additional, Broehl, Andreas, additional, Cancho-Grande, Yolanda, additional, Elowe, Nadine, additional, Henninger, Kerstin, additional, Johannes, Sarah, additional, Jungmann, Natalia, additional, Krainz, Tanja, additional, Lindner, Niels, additional, Maassen, Stefanie, additional, MacDonald, Bryan, additional, Menshykau, Denis, additional, Mittendorf, Joachim, additional, Sanchez, Guzman, additional, Schaefer, Martina, additional, Stefan, Eric, additional, Torge, Afra, additional, Xing, Yi, additional, and Zubov, Dmitry, additional

Published
2024
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3. Synthetic Tigliane Intermediates Engage Thiols to Induce Potent Cell Line Selective Anti‐Cancer Activity

Author

Chow, Sharon, primary, Krainz, Tanja, additional, Bettencourt, Christian J., additional, Broit, Natasa, additional, Ferguson, Blake, additional, Zhu, Mingzhao, additional, Hull, Kenneth G., additional, Pierens, Gregory K., additional, Bernhardt, Paul V., additional, Parsons, Peter G., additional, Romo, Daniel, additional, Boyle, Glen M., additional, and Williams, Craig M., additional

Published
2020
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14. Rhodium-Catalyzed [4+3] Cycloaddition to Furans: Direct Access to Functionalized Bicyclo[5.3.0]decane Derivatives.

Author

Krainz, Tanja, Chow, Sharon, Korica, Natasa, Bernhardt, Paul V., Boyle, Glen M., Parsons, Peter G., Davies, Huw M. L., and Williams, Craig M.

Subjects
*BICYCLODECENES, *RHODIUM, *CARBOXYLATES, *FURANS synthesis, *PROTEIN kinase C
Abstract

An efficient method to directly access the bicyclo[5.3.0]decane core was achieved by rhodium-catalyzed reaction of a novel donor-acceptor cyclopentenyl diazocarboxylate with a variety of furans. As this motif is commonly found within bioactive antitumor natural products, selected systems were further manipulated and evaluated against cancer cell lines sensitive to protein kinase C (PKC) activation. [ABSTRACT FROM AUTHOR]

Published
2016
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16. Synthetic Tigliane Intermediates Engage Thiols to Induce Potent Cell Line Selective Anti-Cancer Activity.

Author

Chow S, Krainz T, Bettencourt CJ, Broit N, Ferguson B, Zhu M, Hull KG, Pierens GK, Bernhardt PV, Parsons PG, Romo D, Boyle GM, and Williams CM

Subjects
Cell Line, Humans, Neoplasms, Phorbols, Protein Kinase C chemistry, Sulfhydryl Compounds chemistry
Abstract

The tigliane ring system, which encompasses iconic members such as phorbol and TPA, is widely renowned due to numerous observations of displaying potent biological activity, and subsequent use as mainstream biochemical tools. Traditionally, naturally occurring phorboids are regarded as tumor promotors through PKC activation, although in recent times more highly oxidized natural derivatives have been identified as anti-tumor agents. In the view that only limited synthetic investigations toward skeletal stereochemical modification have been undertaken, non-natural systems could be useful for a better understanding of the tigliane pharmacophore via interrogation of cellular sensitivity. In this context the concise construction of a number of highly functionalized non-natural D-ring inverted phorbol esters were synthesized, via a rhodium-catalyzed [4+3] cycloaddition, and biologically evaluated using a range of cancer cell lines. The biological results highlight the notion that subtle changes in structure have dramatic effects on potency. Furthermore, although the non-natural derivatives did not outcompete the natural systems in the PKC-activation sensitive MCF7 cancer cell line, they outperformed in other cancer cell lines (MM96L and CAL27). This observation strongly suggested an alternate mode of action not involving activation of PKC, but instead involves thiol addition as indicated by glutathione addition and NF-κB reporter activity., (© 2020 Wiley-VCH GmbH.)

Published
2020
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